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Assay Detail

CHEMBL3829834

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer's Disease Agents.
Montanari S, Scalvini L, Bartolini M, Belluti F, Gobbi S, Andrisano V, Ligresti A, Di Marzo V, Rivara S, Mor M, Bisi A, Rampa A.
J Med Chem (2016) 59 : 6387 -6406
PubMed 27309570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.62 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3827288 1 9.57
CHEMBL3827610 1 9.55
CHEMBL3827044 1 9.28
CHEMBL128390 1 9.16
CHEMBL3828693 1 9.10
CHEMBL440526 1 8.87
CHEMBL3828696 1 7.80
CHEMBL3828443 1 7.15
CHEMBL3827284 1 7.11
CHEMBL3826998 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3827288 IC50 = 0.27 nM 9.57
CHEMBL3827610 IC50 = 0.28 nM 9.55
CHEMBL3827044 IC50 = 0.53 nM 9.28
CHEMBL128390 IC50 = 0.69 nM 9.16
CHEMBL3828693 IC50 = 0.79 nM 9.10
CHEMBL440526 IC50 = 1.36 nM 8.87
CHEMBL3828696 IC50 = 15.9 nM 7.80
CHEMBL3828443 IC50 = 71.2 nM 7.15
CHEMBL3827284 IC50 = 78.2 nM 7.11
CHEMBL3826998 IC50 = 122000.0 nM -